For research use only. Not for therapeutic Use.
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity[1].
NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation (IC50 26.8 nM in HEK293 cells)[2].
NE 52-QQ57 (Compound 13) shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid for 20 days[1].
NE 52-QQ57 (30 mg/kg bid po for 4 days) also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund’s adjuvant model[1].
| Catalog Number | I019640 |
| CAS Number | 1401728-56-0 |
| Synonyms | 2-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-5-piperidin-4-yl-1,3,4-oxadiazole |
| Molecular Formula | C24H28N6O |
| Purity | ≥95% |
| InChI | InChI=1S/C24H28N6O/c1-4-21-20(22-26-15(2)13-16(3)30(22)29-21)14-17-5-7-18(8-6-17)23-27-28-24(31-23)19-9-11-25-12-10-19/h5-8,13,19,25H,4,9-12,14H2,1-3H3 |
| InChIKey | HXPQWNPLNIEJOW-UHFFFAOYSA-N |
| SMILES | CCC1=NN2C(=CC(=NC2=C1CC3=CC=C(C=C3)C4=NN=C(O4)C5CCNCC5)C)C |
| Reference | [1]. Velcicky J, et al. Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis. J Med Chem. 2017 May 11;60(9):3672-3683. [2]. Hosford PS, et al. CNS distribution, signalling properties and central effects of G-protein coupled receptor 4. Neuropharmacology. 2018 Aug;138:381-392. |
